Lomexin® [Fenticonazole]

Pharmacological properties

Pharmacodynamic parameters. the active pharmaceutical ingredient lomexin fenticonazole is a differentiated derivative of imidazole whose unique dechlorinated structure exhibits the fungicidal effect of a wide spectrum of dermatophytes (all types of trichophyton, microsporum, epidermophyton), yeast, other pathogens of mycoses of the mucous membranes, skin and its derivatives, as well as protozoa and gramosa bacteria.

The multimodal mechanism of action of fenticonazole against Candida species includes:

1. Inhibition of secreted aspartate proteases, which prevents the growth, adhesion and penetration of Candida spp. and, accordingly, a clinically significant reduction in relapse rates.

2. Inhibition of the fungal enzyme cytochrome P450 3A - lanosine-14α-demethylase, responsible for the conversion of lanosterol to ergosterol, the main sterol that determines the integrity of the fungal cell membrane and the survival of its cells.

3. Inhibition of additional oxidase and peroxidase enzymes, leading to structural and functional disorders in the fungal cell.

Fenticonazole also exhibits antibacterial activity, the spectrum of which includes gram-positive bacteria (such as Staphylococcus aureus, Staphylococcus aureus, streptococci), a common cause of skin and vaginal superinfection, and protozoa (Trichomonas) by inhibiting the pyruvate oxidoreductase enzyme responsible for cell division or replication. As a drug of the imidazole class, fenticonazole is also active against Gardnerella vaginalis.

Fenticonazole does not affect the release and activity of histamine, epinephrine, norepinephrine, and acetylcholine, as well as vital signs such as blood pressure, heart rate, and lung ventilation.

Pharmacokinetic parameters. The drug lingers in the stratum corneum for a long time and accumulates in the mucous membrane as an active substance for up to 72 hours, forming a “reservoir”. In addition, the drug is poorly absorbed into the systemic circulation through the mucous membrane and skin.

Lomexin did not demonstrate mutagenic properties, hypersensitivity potential, photoallergic and phototoxic effects, as well as negative effects on gonads and reproductive functions.

Indications

Vaginal cream, capsules 200 mg / 600 mg: genital candidiasis, mixed vaginal infections (1000 mg capsules also vaginal trichomoniasis and mixed infections of the mucous membranes of the genital tract of trichomonas and candidiasis etiology).

Cream: dermatophytic skin mycoses (Trichophyton, Microsporum, Epidermophyton) or candida etiology; paronychia, onychia; balanoposthitis, balanitis; erythrasma; pityriasis versicolor; mycoses with superinfection with gram-positive bacteria; dry dandruff and seborrhea.

Application

Capsules 200 mg / 600 mg are administered deeply intravaginally in the supine position 1 time per day at bedtime. the course of treatment is 3 days (or as directed by the doctor); when using 600 mg capsules after 3 days of therapy, in case of symptoms, another 1 capsule is allowed.

At the same time, the patient’s sexual partner applies Lomexin cream (on the penis and foreskin).

Capsules 1000 mg: administered one capsule deeply intravaginally in a horizontal position at bedtime once. In case of trichomonas infection or infection of trichomonas candidiasis etiology, if necessary, 1 capsule of 1000 mg is administered repeatedly in a day. In the treatment of candidal infection with the preservation of the manifestations of the disease, the introduction of 1 capsule of 1000 mg is repeated after 3 days.

Vaginal cream 2%: before going to bed, the contents of one applicator are administered deeply intravaginally in the supine position with the knees bent and legs apart. Possible additional use in the morning if necessary. The applicator must be clean.

The applicator is screwed onto the tube instead of the cap, filled completely (unless otherwise indicated by the doctor) by lightly compressing the tube. After removing the applicator, the cap is immediately screwed onto the tube. After intravaginal administration of the applicator, the piston is lowered and then no manipulations are performed with it until the applicator is removed.

Simultaneous topical therapy is needed at the sexual partner (apply cream on the head of the penis and foreskin).

Cream 2% is distributed over the affected areas of the skin and its folds, the mucous membrane with surface rubbing or lubricating movements 1-2 times a day (depending on the severity of the pathology). The damaged area is pre-washed and dried, the remains of the damaged skin and its appendages are removed.

With a fungal infection of the nails, the cream is combined with an occlusive dressing.

The drug should also be used by the patient’s sexual partner. The duration of therapy is determined by the doctor (determined by the volume and nature of the damage).

Contraindications

Hypersensitivity to the active substance of the drug or its other components.

Side effects

Vaginal forms - a burning sensation in the vaginal mucosa; hyperemia, itching, rash.

Cream 2% - hyperemia, itching, rashes, including erythematous, skin irritation, burning sensation.

special instructions

When using, there is the likelihood of a non-permanent inconsequential burning sensation in the affected areas of the skin or on the mucous membrane at the injection site.

With prolonged use, the development of sensitization or the appearance of insensitive microorganisms is likely, which requires completion of drug therapy and medical advice.

Certain additional ingredients of the drug can cause local reactions on the skin (irritation, contact dermatitis and others) or on the mucous membrane, which also require completion of drug therapy.

Follow the instructions for use of the drug.

If serious adverse reactions have developed or the manifestations of the disease persist for 7 days of drug therapy (or resume), a doctors consultation is necessary.

Before using vaginal cream, make sure the applicator is perfectly clean; after use, rinse it in soapy warm water. If it is necessary to sterilize the applicator, do not use organic solvents or hot water (50 ° C) for this purpose. The applicator is kept dry in the container.

Vaginal forms are not used in conjunction with barrier methods of contraception.

Simultaneous therapy of the sexual partner is necessary in case of infection.

Cream 2% - exclusively for external use. Protect eyes from cream, in case of contact, rinse carefully with plenty of water.

During pregnancy and lactation, as well as in childhood, do not use.

It does not affect the reaction rate when driving vehicles and other mechanisms.

Interactions

The components of vaginal forms - oils and fat-containing substances can cause damage to latex products.

Overdose

Not found. with per os, vomiting and abdominal pain are possible.

Storage conditions

In a place inaccessible to children, at a temperature of ≤25 ° C. vaginal cream must be used within 30 days from the first opening of the tube.